摘要
目的:优化胃舒原位凝胶的成型处方,并对释放度进行研究。方法:以胶凝温度和黏附力为指标,筛选了温敏型原位凝胶的成型基质配比、载药量、生物黏附材料种类及用量,确定了最优成型工艺,并考察了最佳处方的热可逆性。通过释放度试验,研究了药物的体外释放规律。结果:优选出以P40716%、P1887.5%为温敏型凝胶基质,1%HPMC为生物黏附材料,载药量为0.8 g·ml-1的成型处方。该处方在50℃以下热可逆性良好。通过释放度试验得出释放度方程为:LnQ=0.915 2Ln(t)+4.293,r=0.959。该模型符合RITGER-PEPPAS方程,证明了该温敏型原位凝胶剂在释放介质中的释药体系是通过Fick扩散和凝胶骨架溶蚀两种机制协同作用的结果。连翘苷在120 min释放度达到93.95%。结论:制成的胃舒原位凝胶具有较高的生物黏附性和良好的工艺重复性,释放性能较好。
OBJECTIVE To optimize Weishu in situ gel forming prescription,and to study on its release property.METHODS Taking the gelling temperature and adhesion as indexes,the temperature-sensitive in situ gel forming matrix ratio,drug loading,bio-adhesive material type and dosage were screened,then the optimal molding process was determined,and the thermal reversibility of the best prescription was examined.The in vitro drug release was also studied by releasing test.RESULTS The best prescription was P40716% and P1887.5%for the temperature-sensitive gel matrix,1%HPMC as bio-adhesive material,and the drug loading was 0.8 g·ml^-1.The prescription had good thermal reversibility below50℃.By releasing test,the equation of its release was obtained：LnQ=0.915 2Ln（t）＋4.293,r=0.959.This model accorded with RITGER-PEPPAS equation,and it proved that the temperature-sensitive in situ gel in the release medium drug release system was the synergistic results through Fick diffusion and gel skeleton corrosion two kinds of mechanism.The release of forsythin at 120 min reached93.95%.CONCLUSION The produced Weishu in situ gel has high bio-adhesive,good process reproducibility and better release characteristics.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2014年第22期1910-1914,共5页
Chinese Journal of Hospital Pharmacy
关键词
原位凝胶
生物黏附
凝胶温度
处方筛选
释放度
in situ gel
bio-adhesive
gel temperature
prescription screening
release
